Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, Oral:
Elmiron: 100 mg [contains fd&c blue #1 aluminum lake, fd&c blue #2 aluminum lake, fd&c red #40 aluminum lake, fd&c yellow #10 aluminum lake]
Pharmacology
Mechanism of Action
Although pentosan polysulfate sodium is a low-molecular weight heparinoid, it is not known whether these properties play a role in its mechanism of action in treating interstitial cystitis; the drug appears to adhere to the bladder wall mucosa where it may act as a buffer to protect the tissues from irritating substances in the urine.
Pharmacokinetics/Pharmacodynamics
Absorption
~6%
Metabolism
Hepatic and splenic via partial desulfation; partial depolymerization occurs in the renal parenchyma; saturable
Excretion
Feces (58% to 84%, as unchanged drug); urine (6%, primarily as metabolites)
Time to Peak
Serum: 2 hours (range: 0.6-120 hours)
Half-Life Elimination
20-27 hours
Use: Labeled Indications
Interstitial cystitis: Relief of bladder pain or discomfort due to interstitial cystitis
Contraindications
Hypersensitivity to pentosan polysulfate sodium, structurally related compounds (LMWHs or heparin), or any component of the formulation
Dosage and Administration
Dosing: Adult
Interstitial cystitis: Oral: 100 mg 3 times daily
Note: Patients should be re-evaluated after 3 months; therapy may continue for an additional 3 months if there has been no improvement and if there are no therapy-limiting side effects. The risks and benefits of continued use beyond 6 months in patients who have not responded is not yet known.
Dosing: Geriatric
Refer to adult dosing.
Dosing: Pediatric
Interstitial cystitis: Adolescents ≥16 years: Oral: Refer to adult dosing.
Administration
Administer with water 1 hour before or 2 hours after meals.
Storage
Store at room temperature of 15°C to 30°C (59°F to 86°F).
Drug Interactions
Agents with Antiplatelet Properties (e.g., P2Y12 inhibitors, NSAIDs, SSRIs, etc.): Pentosan Polysulfate Sodium may enhance the adverse/toxic effect of Agents with Antiplatelet Properties. Specifically, the risk of bleeding may be increased by concurrent use of these agents. Monitor therapy
Anticoagulants: Pentosan Polysulfate Sodium may enhance the anticoagulant effect of Anticoagulants. Monitor therapy
Adverse Reactions
1% to 10%:
Central nervous system: Headache (3%), dizziness (1%)
Dermatologic: Alopecia (4%), skin rash (3%)
Gastrointestinal: Diarrhea (4%), nausea (4%), abdominal pain (2%), dyspepsia (2%)
Hematologic & oncologic: Rectal hemorrhage (6%)
Hepatic: Abnormal hepatic function tests (1%; dose-related)
<1%, postmarketing, and/or case reports: Amblyopia, anemia, anorexia, colitis, conjunctivitis, constipation, dehydration, depression, diaphoresis, dyspnea, ecchymoses, emotional lability, epistaxis, esophagitis, flatulence, gastritis, gingival hemorrhage, hyperkinetic muscle activity, hypersensitivity reaction, insomnia, leukopenia, maculopathy (Hanif 2019), optic neuritis, oral mucosa ulcer, pharyngitis, prolonged partial thromboplastin time, prolonged prothrombin time, pruritus, retinal hemorrhage, rhinitis, skin photosensitivity, thrombocytopenia, tinnitus, urticaria, vomiting
Warnings/Precautions
Concerns related to adverse effects:
- Bleeding: Pentosan polysulfate is a low-molecular weight heparin-like compound with anticoagulant and fibrinolytic effects, therefore, bleeding complications (such as ecchymosis, epistaxis, and gum bleeding) may occur. Patients undergoing invasive procedures or having signs or symptoms of underlying coagulopathies or other increased risk of bleeding (eg, receiving heparin, warfarin, thrombolytics, NSAIDs, or high dose aspirin) should be evaluated prior to use.
Disease-related concerns:
- Aneurysm: Carefully evaluate patients with aneurysm before initiating therapy.
- Bleeding disorders: Carefully evaluate patients with hemophilia and/or thrombocytopenia before initiating therapy.
- Gastrointestinal disease: Carefully evaluate patients with gastrointestinal ulcerations, polyps, and/or diverticula before initiating therapy.
- Heparin-induced thrombocytopenia: Use with caution in patients with a history of heparin-induced thrombocytopenia.
- Hepatic impairment: Use with caution in patients with hepatic impairment.
Special populations:
- Pediatric: Safety and efficacy have not been established in children <16 years of age.
Pregnancy
Pregnancy Considerations
No adverse events were noted in animal reproduction studies; however, reversible limb bud abnormalities were noted during in vitro animal studies. There are no adequate and well-controlled studies in pregnant women. Use with caution and only if clearly needed during pregnancy. Based on limited data, pentosan polysulfate does not appear to cross the placenta.
Patient Education
What is this drug used for?
- It is used to ease pain, swelling, and irritation of the bladder.
Frequently reported side effects of this drug
- Nausea
- Dizziness
- Diarrhea
- Headache
- Hair loss
Other side effects of this drug: Talk with your doctor right away if you have any of these signs of:
- Bleeding like vomiting blood or vomit that looks like coffee grounds; coughing up blood; blood in the urine; black, red, or tarry stools; bleeding from the gums; abnormal vaginal bleeding; bruises without a reason or that get bigger; or any severe or persistent bleeding.
- Signs of a significant reaction like wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat.
Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.
Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a brief summary of general information about this medicine. It does NOT include all information about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not specific medical advice and does not replace information you receive from the healthcare provider. You must talk with the healthcare provider for complete information about the risks and benefits of using this medicine.
